Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/37—Esters of carboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/35—Ketones, e.g. benzophenone
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
  • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/37—Esters of carboxylic acids
  • A61K8/375—Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
  • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/004—Aftersun preparations

Definitions

• the invention relates to a therapeutic composition and its use in the treatment or prevention of certain skin disorders, and more particularly to the use of an a 2-hydroxyalkanoic acid, or an ester thereof, together with a sunscreen active ingredient, in the preparation of therapeutic compositions for the treament or prevention of a specified skin disorder.
• the therapeutic composition is intended for topical application to human skin, particularly to treat and/or to prevent desquamation which can follow excessive exposure of the skin to sunlight.
• the therapeutic composition can furthermore reduce erythema which can also result from excessive exposure of the human skin to sunlight.
• Treatment of the skin with a sunscreen prior to exposure to sunlight can prevent, or at least limit, erythema.
• sunscreens have little or no effect on subsequent skin peeling (desquamation).
• Conventional treatment of skin following over-exposure to sunlight usually involves topical application of a moisturiser such as an oil-in-water cream, but this will generally only provide a cooling effect with some relief of the burning and itching sensation that accompanies erythema. Usually it will not prevent peeling of the skin.
• compositions containing both a 2-hydroxyalkanoic acid, or an ester thereof, and a sunscreen active ingredient can be used in the treatment and/or prevention of sun-induced desquamation.
• the invention provides for the use of a 2-hydroxyalkanoic acid, or an ester thereof, having the structure:
• R is --H, C 2-10 alkyl or a monoglyceride, diglyceride or triglyceride residue
• n 0, or an integer of from 1 to 27,
• the inventions also provides a therapeutic composition for alleviating or preventing skin damage characterised by sun-induced desquamation, which composition comprises as active ingredients a therapeutically effective amount of a desquamation inhibitor chosen from 2-hydroxyalkanoic acids and esters thereof, as hereinbefore defined, and a mixture thereof, together with a sunscreen active ingredient, or a mixture thereof, in a therapeutically acceptable vehicle for topical application.
• a desquamation inhibitor chosen from 2-hydroxyalkanoic acids and esters thereof, as hereinbefore defined, and a mixture thereof, together with a sunscreen active ingredient, or a mixture thereof, in a therapeutically acceptable vehicle for topical application.
• the invention also provides a method for alleviating the symptoms of sun-induced desquamation comprising topically applying to involved areas of the body an effective amount of a composition comprising as active ingredients, a 2-hydroxyalkanoic acid or an ester thereof, as hereinbefore defined, or a mixture thereof, together with a sunscreen active ingredient, or a mixture thereof, in a therapeutically acceptable vehicle for topical application.
• the invention also provides for the use of a therapeutic composition
• a therapeutic composition comprising as active ingredients a 2-hydroxyalkanoic acid or an ester thereof, as hereinbefore defined, or a mixture thereof, together with a sunscreen active ingredient, or a mixture thereof, in the treatment or prevention of sun-induced desquamation.
• the therapeutic composition of the invention comprises a 2-hydroxyalkanoic acid or an ester thereof having the structure:
• R is --H, C 2-10 alkyl or a monoglyceride, diglyceride or triglyceride residue
• n 0, or an integer of from 1 to 27.
• 2-hydroxyalkanoic acids examples include:
• Preferred 2-hydroxyalkanoic acids are 2-hydroxypropanoic, 2-hydroxyhexanoic acid and 2-hydroxyoctanoic acid.
• esters of 2-hydroxyalkanoic acids include:
• the amount of 2-hydroxyalkanoic acid or ester thereof to be employed in accordance with the invention will normally be from 0.1 to 20%, preferably from 0.5 to 10% and most preferably from 0.5 to 2% by weight of the therapeutic composition.
• the sunscreen active ingredient is a mixture of the sunscreen active ingredient
• the therapeutic composition of the invention also comprises one or more sunscreen active ingredients.
• sunscreen active ingredients include:
• Glyceryl p-aminobenzoic acid such as Escalol 106
• Homomenthyl salicylate such as Filtrosol A
• Ethylhexyl p-methoxycinnamate (such as Parsol MCX).
• Butylmethoxydibenzoylmethane (such as Parsol 1789)
• the amount of the sunscreen active ingredient to be employed in accordance with the invention will normally be from 0.01 to 10%, preferably from 0.1 to 5% and most preferably from 1 to 5% by weight of the therapeutic composition.
• the therapeutic composition of the invention also comprises a therapeutically acceptable vehicle, usually in the form of a lotion, cream, ointment, gel, powder, solid stick or aerosol concentrate formed from cosmetically acceptable ingredients as conventionally employed in the art.
• a therapeutically acceptable vehicle usually in the form of a lotion, cream, ointment, gel, powder, solid stick or aerosol concentrate formed from cosmetically acceptable ingredients as conventionally employed in the art.
• the amount of the therapeutically acceptable vehicle to be employed in accordance with the invention will normally form the balance of the therapeutic composition after taking account of the 2-hydroxyalkanoic acid and/or ester thereof, the sunscreen active ingredient and optional ingredients. Accordingly, the therapeutically acceptable vehicle with normally form from 50 to 99.89%, preferably from 70 to 99.4% by weight of the therapeutic composition.
• the therapeutic composition according to the invention can also optionally contain further ingredients in addition to those which are conventionally used for the provision of the therapeutically acceptable vehicle.
• the therapeutic composition can optionally comprise further ingredients such as a perfume, colourant, preservative, antioxidant, emollient or aerosol propellant.
• the therapeutic composition of the invention can be prepared in the form of a solution, lotion, gel, cream, ointment, solid stick, aerosol or powder, or in any other form suited to administration topically to human skin.
• the therapeutic composition is a liquid, such as a lotion or aerosol, or a semi-liquid such as a gel, cream or ointment, or a solid stick
• a liquid such as a lotion or aerosol, or a semi-liquid such as a gel, cream or ointment, or a solid stick
• a suitable cream or ointment base containing, for example an oil or silicone oil and water, or stick base containing a gelling agent such as
• the therapeutic composition is a powder
• a powder diluent such as talc, starch, kaolin, Fuller's earth or other suitable powder base
• therapeuticly acceptable carriers diluents or emollients
• emollients can be incorporated in the therapeutic composition according to the invention, in order to facilitate even distribution over the affected area of the skin at a concentration or dosage suitable for treatment or prevention of the sun-induced desquamation.
• the aqueous phase should have a pH value of from 2 to 9, preferably 3 to 6 and ideally from 4 to 5.
• compositions having a pH value of less than 2 are likely to be effective in the treatment or prevention of sun-induced desquamation, topical application of such compositions has been found to produce stinging, burning or irritation.
• Therapeutic compositions having a pH value of greater than 9 are likely to exhibit reduced effectiveness in the treatment or prevention of sun-induced desquamation.
• pH adjustant Any suitable therapeuticly acceptable pH adjustant can be employed to set the pH of the composition at a desired value.
• pH adjustants include alkanolamines, especially triethanolamine and buffers such as lactic acid/triethanolamine lactate.
• the invention also provides a method for the treatment or prevention of sun-induced desquamation in man, which method of treatment comprises applying to involved areas of the skin a therapeutically effective amount of a composition comprising from 0.1 to 20% by weight of the 2-hydroxyalkanoic acid and/or ester thereof and from 0.01 to 10% by weight of the sunscreen agent, together with a therapeutically acceptable vehicle.
• a therapeutically effective amount of the composition according to the invention which can be applied topically to human skin in order to reduce or prevent the occurence of sun-induced desquamation will be from 0.1 g to 1 g over an area of skin of 100 sq cm. This amount conveniently can be applied once or twice daily, in particular before exposure to sunlight. Higher or lower doses can be applied if desired.
• One female subject whose arms are habitually subject to severe sunburn and desquamation following exposure to sunlight was treated prophilactically by applying to the left arm a composition containing 2-hydroxyoctanoic acid (1%) and a sunscreen (Parsol 1789 1%), and to the other arm a conventional oil-in-water moisturising lotion.
• the therapeutic compositions prepared according to the method defined by this invention are accordingly useful prophilactically in preventing the onset of sun-induced desquamation especially if applied topically to skin before exposure to sunlight, and also in the prevention of sun-induced desquamation after exposure to excessive amounts of sunlight and following development of erythema.
• This example illustrates the formulation of a therapeutic sunburn lotion according to the invention.
• This example illustrates the formulation of a therapeutic sunburn cream according to the invention.
• This example illustrates the formulation of a therapeutic pre-sun lotion according to the invention.
• the water-in-oil (w/o) base employed had the following formulation:
• This example illustrate the formulation of a therapeutic pre-sun lotion according to the invention based on the water-in-oil (w/o) base of Example 8.
• This example illustrates a therapeutic sunburn cream according to the invention based on the water-in-oil (w/o)
• This example illustrates a therapeutic sunburn cream according to the invention based on the water-in-oil (w/o) base of Example 8.
• compositions described in the above examples can be used as pre-sun or post-sunburn treatment for the prevention of alleviation of sun-induced skin peeling and for reducing or eliminating erythema.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• General Health & Medical Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• Animal Behavior & Ethology (AREA)
• Birds (AREA)
• Epidemiology (AREA)
• Emergency Medicine (AREA)
• Dermatology (AREA)
• Cosmetics (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicinal Preparation (AREA)

Applications Claiming Priority (2)

Publications (1)

Family

ID=10603383

Family Applications (1)

Country Status (12)

Cited By (10)

Families Citing this family (25)

Citations (8)

Family Cites Families (3)

• 1986
  • 1986-08-29 GB GB868620896A patent/GB8620896D0/en active Pending
• 1987
  • 1987-08-24 CA CA000545155A patent/CA1299109C/fr not_active Expired - Fee Related
  • 1987-08-24 PH PH35720A patent/PH24883A/en unknown
  • 1987-08-25 US US07/089,210 patent/US4839161A/en not_active Expired - Fee Related
  • 1987-08-25 AU AU77395/87A patent/AU598020B2/en not_active Ceased
  • 1987-08-27 JP JP62214125A patent/JPS6368519A/ja active Pending
  • 1987-08-27 ES ES87307589T patent/ES2040257T3/es not_active Expired - Lifetime
  • 1987-08-27 AT AT87307589T patent/ATE66139T1/de not_active IP Right Cessation
  • 1987-08-27 DE DE8787307589T patent/DE3772139D1/de not_active Revoked
  • 1987-08-27 ZA ZA876403A patent/ZA876403B/xx unknown
  • 1987-08-27 EP EP19870307589 patent/EP0261812B1/fr not_active Expired - Lifetime
• 1991
  • 1991-10-10 GR GR91401528T patent/GR3002880T3/el unknown

Patent Citations (10)

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